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1. 发明申请

US20050197338A1 Substituted pyrazole urea compounds for the treatment of inflammation 审中-公开
标题翻译：用于治疗炎症的取代的吡唑脲化合物
公开(公告)号：US20050197338A1
公开(公告)日：2005-09-08
申请号：US10970769
申请日：2004-10-21
申请人： He Huang , Michael Stealey , Gunnar Hanson , Patrick Lennon , Bruce Hamper , Jin Xie , David Oburn , Serge Wolfson , Theresa Fletcher , Richard Heier , Matthew Reding , Michael Clare
发明人： He Huang , Michael Stealey , Gunnar Hanson , Patrick Lennon , Bruce Hamper , Jin Xie , David Oburn , Serge Wolfson , Theresa Fletcher , Richard Heier , Matthew Reding , Michael Clare
IPC分类号： A61K31/415 , A61K31/416 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , C07D231/38 , C07D231/40 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10
CPC分类号： C07D403/10 , C04B35/632 , C07D231/38 , C07D401/12 , C07D403/04 , C07D405/10 , C07D409/10 , C07D413/10
摘要： Compounds of Formula I: wherein X1, X2, L1, A, R, L2, R1, R12, R12a, R13, R14 and R14a are as defined herein, are disclosed.
摘要翻译：式I的化合物：其中X 1，X 2，L 1，A，R，L 2， R 1，R 12，R 12，R 13，R 14和R 14，和 R 14a如本文所定义。

2. 发明申请

US20050256180A1 Substituted pyrazolyl compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代的吡唑基化合物
公开(公告)号：US20050256180A1
公开(公告)日：2005-11-17
申请号：US11113926
申请日：2005-04-25
申请人： Arija Bergmanis , Michael Clare , Joyce Crich , Lifeng Geng , Timothy Hagen , Gunnar Hanson , Stephen Houdek , He Huang , Donna Iula , Francis Koszyk , Shuyuan Liao , Scott Mohler , Maria Nguyen , Richard Partis , Michael Stealey , Michael Tollefson , Richard Weier , Xiangdong Xu , Dominique Bonafoux , Theresa Fletcher , Bruce Hamper , Patrick Lennon , Subo Liao , Suzanne Metz , David Oburn , Thomas Owen , Angela Scates , Michael Vazquez , Serge Wolfson
发明人： Arija Bergmanis , Michael Clare , Joyce Crich , Lifeng Geng , Timothy Hagen , Gunnar Hanson , Stephen Houdek , He Huang , Donna Iula , Francis Koszyk , Shuyuan Liao , Scott Mohler , Maria Nguyen , Richard Partis , Michael Stealey , Michael Tollefson , Richard Weier , Xiangdong Xu , Dominique Bonafoux , Theresa Fletcher , Bruce Hamper , Patrick Lennon , Subo Liao , Suzanne Metz , David Oburn , Thomas Owen , Angela Scates , Michael Vazquez , Serge Wolfson
IPC分类号： A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61P19/02 , A61P25/04 , A61P29/00 , A61P35/00 , C07D231/54 , C07D333/62 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/4162
CPC分类号： C07D403/12 , C07D231/54 , C07D333/62 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
摘要翻译：本发明涉及取代的吡唑基衍生物，包含这些的组合物，中间体，制备取代的吡唑基衍生物的方法，以及用于治疗癌症，炎症和炎症相关疾病如关节炎的方法。

3. 发明申请

US20050054871A1 Process for the preparation of N-phosphonomethylglycine and derivatives thereof 有权
标题翻译： N-膦酰基甲基甘氨酸及其衍生物的制备方法
公开(公告)号：US20050054871A1
公开(公告)日：2005-03-10
申请号：US10924265
申请日：2004-08-23
申请人： James Coleman , Jerry Ebner , Eric Haupfear , Patrick Lennon , Joseph Schaper , Samuel Tremont , Serge Wolfson , Philip Brodsky
发明人： James Coleman , Jerry Ebner , Eric Haupfear , Patrick Lennon , Joseph Schaper , Samuel Tremont , Serge Wolfson , Philip Brodsky
IPC分类号： C07F9/28 , C07F9/38
CPC分类号： C07F9/3813 , Y02P20/582
摘要： N-phosphonomethylamines are produced by reaction of an amine substrate with a halomethylphosphonic acid or salt thereof, a hydroxymethylphosphonic acid or salt thereof, or a dehydrated self-ester dimer, trimer or oligomer of hydroxymethylphosphonic acid. Among the products that may be prepared according to the process are N-phosphonomethylaminocarboxylic acids such as (e.g.) glyphosate, N-phosphonomethylaminoalkanols such as (e.g.) hydroxyethlaminomethylphosphonic acid, and N-acylaminomethylphosphonic acids such as (e.g.) N-carbamylaminomethylphosphonic acid. Certain reactions are conducted with a substantial excess of amine reactant in order to drive the conversion while avoiding excessive formation of bis(N-phosphonomethyl)amine by-products. Other reactions use a secondary amine substrate (such as iminodiacetic acid) and can be conducted at substantial equimolar ratios of halomethylaminomethylphosphonic acid or hydroxyaminomethylphosphonic acid to secondary amine reactant without significant formation of bis(phosphonomethyl)amine by-products. Further disclosed is a process for the preparation of hydroxymethylphosphonic acid self-ester dimers, trimers and oligomers by azeotropic dehydration.
摘要翻译： N-膦酰基甲胺通过胺底物与卤甲基膦酸或其盐，羟甲基膦酸或其盐或羟甲基膦酸的脱水的自酯二聚物，三聚体或低聚物的反应来制备。可根据该方法制备的产物是N-膦酰基乙基氨基羧酸，例如（例如）草甘膦，N-膦酰基甲基氨基链烷醇如（例如）羟基乙基氨基甲基膦酸和N-酰基氨基甲基膦酸如（例如）N-氨基甲酰基氨基甲基膦酸。某些反应用大量过量的胺反应物进行，以驱动转化，同时避免过度形成双（N-膦酰基甲基）胺副产物。其他反应使用仲胺底物（例如亚氨基二乙酸），并且可以以基本上等摩尔比率的卤代甲基氨基甲基膦酸或羟基氨基甲基膦酸与仲胺反应物进行反应，而不显着形成双（膦酰基甲基）胺副产物。进一步公开了通过共沸脱水制备羟甲基膦酸自酯二聚体，三聚体和低聚物的方法。

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